Double-blinded, Controlled, Randomized Study of Dihydrocodeine Tartrate vs Codeine Phosphate in Treating Cancer Pain

To compare the effects and adverse reactions of dihydrocodeine tartrate andcodeine phosphate in treating moderate cancer pain. Methods: Sixty-nine cases of cancer patientswith moderate pain were treated with dihydrocodeine tartrate or codeine phosphate respectively bydouble-blind, controlled randomized methods and the effects and adverse reactions were observed.Results: After administration of dihydrocodeine tartrate or codeine phosphate, in treatment group orcontrol group, the total effective rate was 86.6% and 93.6%, and common adverse symptoms includedconstipation (31.3%/12.9%), nausea (18.8%/19.7%), gastric trouble (18.8%/19.7%), skin pruritus(12.5%/10%), vomit (9.3% and 6.5%) with the difference being not significant. Conclusion: Theeffects of dihydrocodeine tartrate in treating moderate cancer pain are similar to codeinephosphate. Both them can be used to treat moderate cancer pain.

Separation and characterization of degradation/interaction products of codeine phosphate in ibuprofen arginate/codeine phosphate combination formulation by HPLC coupled with MS analysis

A simple HPLC method was developed and validated according to the ICH guidelines to detect and quantify the related substances of codeine phosphate in the raw material and in its combination formulation with ibuprofen before and after forced degradation. These products were further identified by using HPLC-TOF/MS and MS/MS techniques. Good separations were obtained on a C18 （250 min×4.6 mm, 5 μm） column maintained at 50 ℃ with linear gradient elution by a mixture of mobile phase A （ammonium acetate （pH 6.0 regulated with acetic acid, 0.04 M）-acetonitrile （92：8, v/v）） and mobile phase B （acetonitrile） at a flow rate of 1 mL/min. UV detection was set at 245 nm. Codeine was found to be instable under oxidation with the production of mainly two stereoisomers of codeine N-oxide. A new degradation product, not reported previously, was detected under alkaline hydrolysis, which was identified as 6-hydroxy-3-methoxy-17-methyl-7,8-didehydromorphinan-5-ol and shortly named as deshydrolevomethorphandiol. The esterification of codeine by ibuprofen occurred in very small amount and only under acidic stress. These results contribute to the understanding of the degradation behavior of codeine and its interaction with ibuprofen. The developed method is sensitive and precise and could be applied for the quality control of codeine bulk drug, preparations of codeine phosphate, and its combination with ibuprofen.

Studies of Active Ingredients in Cough Syrup by Capillary Zone Electrophoresis with Amperometric Detection

The present paper covers a simple, reliable and reproducible method, based on capillary zone electrophoresis(CZE) with amperometric detection(AD), for the separation and the determination of ephedrine hydrochloride, promethazine hydrochloride and codeine phosphate. Under the optimal conditions, the three analytes were base-line separated completely within 16 min. Good linear relationships between the peak heights and the concentrations of the three analytes were obtained with the correlation coefficients better than 0 9993. The method was directly applied to the determination of the active ingredients in pharmaceutical preparations and the assay results were satisfactory.